INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo CLOPIXOL® TABLETS 2 mg
CLOPIXOL® TABLETS 10 mg

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form):

CLOPIXOL® TABLETS 2 mg
CLOPIXOL® TABLETS 10 mg

COMPOSITION:
Each tablet contains
zuclopenthixol dihydrochloride equivalent to 2 mg or 10 mg zuclopenthixol.

PHARMACOLOGICAL CLASSIFICATION:
A 2.6.5 Thioxanthenes

PHARMACOLOGICAL ACTION:
CLOPIXOL is a thioxanthene derivative with pronounced antipsychotic and specific dampening effect. The antipsychotic effect of neuroleptics is normally related to their dopamine receptor blocking effect, which seems to release a chain reaction as other transmitter systems are influenced as well.
The bioavailability after oral administration is 25-40%. Maximum serum concentration is reached after about 4 hours. Highly significant correlations exist between the dose and the area under the serum concentration curves. CLOPIXOL is distributed in the organism in the same way as seen for other neuroleptics with the highest concentrations of drug and metabolites in liver, lung, intestines and kidneys and lower concentrations in heart, spleen and brain. Autoradiographic studies in mice show that small amounts of radioactive labelled drug and/or metabolites cross the placenta barrier and that some radioactivity is excreted with milk. The metabolism proceeds along three main routes - sulphoxidation, side chain N - dealkylation and glucuronic acid conjugation. The metabolites are not psychopharmacologically active. The biological half-life in humans is about 20 hours. The elimination proceeds mainly with faecal excretion being 8-11 times urinary excretion in rats.

INDICATIONS:
Symptoms of restlessness, agitation, hostility, aggression, psychomotor excitement and other behavioural disturbances in acute and chronic schizophrenia, manic phase of bipolar affective disorder, senile and arteriosclerotic dementia and mental retardation.

CONTRA-INDICATIONS:
Acute alcohol, barbiturate and opiate intoxications, comatose states.

WARNINGS:
Patients on long-term therapy should be watched carefully. CLOPIXOL should be used with caution in patients with convulsive disorders or advanced hepatic, renal or cardiovascular disease. In common with other therapies, it is recommended that CLOPIXOL should not be administered during pregnancy, particularly the first trimester, unless the importance of control of psychotic symptoms outweighs the theoretical hazards of foetal malformation. The ability to drive a car or operate machinery may be affected. Therefore, caution should be exercised initially, until the individual’s reaction to treatment is known.

DOSAGE AND DIRECTIONS FOR USE:
Dosage should be individually adjusted according to the condition. In general, small doses should be used initially and increased to the optimal effective level as rapidly as possible based on therapeutic responses. The maintenance dose can usually be given as a single dose at bedtime.
Acute schizophrenia and other acute psychoses. Severe acute states of agitation. Mania.
Usually 10-50 mg/day.
In moderate to severe cases initially 20 mg/day increased, if necessary, by 10-20 mg/day every 2-3 days to 75 mg.
Chronic schizophrenia and other chronic psychoses.
Maintenance dosage usually 20-40 mg/day.
Agitation in oligophrenic patients.
6-20 mg/day, if necessary increased to 25-40 mg daily.
Agitation and confusion in senile patients.
2-6 mg/day, which can be administered late in the day. If necessary increased to 10-20 mg/day.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects
Extrapyramidal: Akinesia, parkinsonism, akathisia and dystonia may occur, especially during the early phase of treatment. In most cases these side-effects can be satisfactorily controlled by reduction of dosage and/or antiparkinsonian drugs. Tardive dyskinesias, which can be more or less persistent, may appear in some patients on long-term therapy. Antiparkinsonian drugs do not alleviate these symptoms. Reduction in dosage or, if possible, discontinuation of therapy is recommended.
Psychic: Drowsiness initially.
Autonomic and cardiovascular: Dry mouth, urinary retention, disturbance of accommodation, obstipation, tachycardia, postural hypotension and dizziness.
Liver: Transient mild alterations in liver function tests may occur.
Interactions:
CLOPIXOL may enhance the response to alcohol and the effects of barbiturates and other CNS depressants. CLOPIXOL should not be given concomitantly with guanethidine or similar acting compounds, since neuroleptics may block the antihypertensive effect of these compounds. CLOPIXOL may lower the effect of adrenergic drugs and concomitant use of metoclopramide and piperazine increases the risk of extrapyramidal symptoms.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Treatment is symptomatic and supportive. Gastric lavage should be carried out immediately and activated charcoal may be administered. Measures aimed at supporting the respiratory and cardiovascular systems should be instituted. Epinephrine must not be used in these patients.

IDENTIFICATION:
CLOPIXOL Tablets 2 mg: Round, biconvex, pale-red, film-coated tablets.
CLOPIXOL Tablets 10 mg: Round, biconvex, light red-brown, film-coated tablets.

PRESENTATION:
Grey plastic containers with 100 tablets.

STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light. Keep out of reach of children.

REGISTRATION NUMBER:
CLOPIXOL® Tablets 2 mg:         T/2.6.5/180
CLOPIXOL® Tablets 10 mg:         T/2.6.5/181

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
H. LUNDBECK (PTY) LTD
P O BOX 2357
RANDBURG
2125

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
3 June 1991

Updated on this site: May 2000

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